Relationship between structure and antibacterial activity of lipophilic N-acyldiamines

Camila G de Almeida; Gabriela D Garbois; Lorena M Amaral; Cláudio C Diniz; Mireille Le Hyaric

doi:10.1016/j.biopha.2009.09.013

Relationship between structure and antibacterial activity of lipophilic N-acyldiamines

Biomed Pharmacother. 2010 Apr;64(4):287-90. doi: 10.1016/j.biopha.2009.09.013. Epub 2009 Nov 5.

Authors

Camila G de Almeida¹, Gabriela D Garbois, Lorena M Amaral, Cláudio C Diniz, Mireille Le Hyaric

Affiliation

¹ Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, 36036-900 Juiz de Fora, MG, Brazil.

PMID: 19942397
DOI: 10.1016/j.biopha.2009.09.013

Abstract

We report in this work the preparation and antibacterial evaluation of a series of N-monoacylated diamines against six Gram-positive and 11 Gram-negative bacteria. The results obtained showed the existence of relationship between lipophilicity and antibacterial activity of the tested compounds. The best results were obtained against Gram-positive bacteria for compounds having a 10-12 carbons alkyl chain. Compound 4e was the most active against Microccus lentus (MIC=2 microg/mL), Staphylococcus aureus ATCC 29213 (MIC=4 microg/mL) and Enterobacter aerogenes CDC 1680 (MIC=8 microg/mL).

MeSH terms

Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology*
Diamines / administration & dosage
Diamines / chemistry
Diamines / pharmacology*
Gram-Negative Bacteria / drug effects
Gram-Positive Bacteria / drug effects
Microbial Sensitivity Tests
Structure-Activity Relationship

Substances

Anti-Bacterial Agents
Diamines